| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1374154 | Bioorganic & Medicinal Chemistry Letters | 2009 | 6 Pages |
Abstract
A series of N-substituted sulfonylamino-alkanecarboxylate ADAMTS-5 (Aggrecanase-2) inhibitors has been synthesized and the in vitro enzyme SAR is discussed. This report is the first example of carboxylate-based ADAMTS-5 inhibitors which show strong potency of IC50 < 0.1 μM with excellent selectivity over MMP-1 and TACE.
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Related Topics
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Chemistry
Organic Chemistry
Authors
Makoto Shiozaki, Katsuya Maeda, Tomoya Miura, Yosuke Ogoshi, Julia Haas, Andrew M. Fryer, Ellen R. Laird, Nicole M. Littmann, Steven W. Andrews, John A. Josey, Takayuki Mimura, Yuichi Shinozaki, Hiromi Yoshiuchi, Takashi Inaba,